385570 | Heat Shock Factor 1 Inhibitor, KRIBB11 - Calbiochem

385570
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃H₁₂N₆O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      385570-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 in a reversible manner and prevents HSF1 from recruiting p-TEFb to the hsp70 promoter site (IC50 ≤3 µM in HCT-116 ChIP assays), a critical step for heat shock-induced transcription activation (IC50 <1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (50 mg/kg i.p.).
          Catalogue Number385570
          Brand Family Calbiochem®
          SynonymsHeat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine , HSF1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II
          References
          ReferencesYoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.
          Product Information
          FormOrange-yellow solid
          Hill FormulaC₁₃H₁₂N₆O₂
          Chemical formulaC₁₃H₁₂N₆O₂
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -20°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          385570

          References

          Reference overview
          Yoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision02-April-2012 JSW
          SynonymsHeat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine , HSF1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II
          DescriptionA cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 (heat shock factor 1) in a reversible manner and prevents HSF1 from recruiting p-TEFb (positive transcription elongation factor b) to the hsp70 promoter site (IC50 ≤3 µM in HCT-116 ChIP assays), a critical step for the p-TEFb CDK9 subunit-catalyzed pol II CTD (RNA polymerase II c-terminal domain) Ser-2 phosphorylation and transcription activation upon heat shock induction (IC50 <1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 ranges from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (by 47.4% on day 31; single i.p. dosage of 50 mg/kg on day 13 after cancer implantation). Does not affect TNF-α-induced NF-κB activity in HeLa or heat shock-induced HSF1 ser230 phosphorylation and promoter association in HCT-116 even at concentrations as high as 10 µM.
          FormOrange-yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₃H₁₂N₆O₂
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml; brown solution)
          Storage -20°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesYoon, Y.J., et al. 2010. J. Biol. Chem. 286, 1737.